General Information of the Protein
Protein ID
PT00897
Protein Name
Potassium voltage-gated channel subfamily H member 2
Secondarily
Protein Name
Eag homolog
Ether-a-go-go-related gene potassium channel 1
Voltage-gated potassium channel subunit Kv11.1
Gene Name
KCNH2
Secondarily
Gene Name
ERG
ERG1
HERG
Sequence
MPVRRGHVAPQNTFLDTIIRKFEGQSRKFIIANARVENCAVIYCNDGFCELCGYSRAEVMQRPCTCDFLHGPRTQRRAAAQIAQALLGAEERKVEIAFYRKDGSCFLCLVDVVPVKNEDGAVIMFILNFEVVMEKDMVGSPAHDTNHRGPPTSWLAPGRAKTFRLKLPALLALTARESSVRSGGAGGAGAPGAVVVDVDLTPAAPSSESLALDEVTAMDNHVAGLGPAEERRALVGPGSPPRSAPGQLPSPRAHSLNPDASGSSCSLARTRSRESCASVRRASSADDIEAMRAGVLPPPPRHASTGAMHPLRSGLLNSTSDSDLVRYRTISKIPQITLNFVDLKGDPFLASPTSDREIIAPKIKERTHNVTEKVTQVLSLGADVLPEYKLQAPRIHRWTILHYSPFKAVWDWLILLLVIYTAVFTPYSAAFLLKETEEGPPATECGYACQPLAVVDLIVDIMFIVDILINFRTTYVNANEEVVSHPGRIAVHYFKGWFLIDMVAAIPFDLLIFGSGSEELIGLLKTARLLRLVRVARKLDRYSEYGAAVLFLLMCTFALIAHWLACIWYAIGNMEQPHMDSRIGWLHNLGDQIGKPYNSSGLGGPSIKDKYVTALYFTFSSLTSVGFGNVSPNTNSEKIFSICVMLIGSLMYASIFGNVSAIIQRLYSGTARYHTQMLRVREFIRFHQIPNPLRQRLEEYFQHAWSYTNGIDMNAVLKGFPECLQADICLHLNRSLLQHCKPFRGATKGCLRALAMKFKTTHAPPGDTLVHAGDLLTALYFISRGSIEILRGDVVVAILGKNDIFGEPLNLYARPGKSNGDVRALTYCDLHKIHRDDLLEVLDMYPEFSDHFWSSLEITFNLRDTNMIPGSPGSTELEGGFSRQRKRKLSFRRRTDKDTEQPGEVSALGPGRAGAGPSSRGRPGGPWGESPSSGPSSPESSEDEGPGRSSSPLRLVPFSSPRPPGEPPGGEPLMEDCEKSSDTCNPLSGAFSGVSNIFSFWGDSRGRQYQELPRCPAPTPSLLNIPLSSPGRRPRGDVESRLDALQRQLNRLETRLSADMATVLQLLQRQMTLVPPAYSAVTTPGPGPTSTSPLLPVSPLPTLTLDSLSQVSQFMACEELPPGAPELPQEGPTRRLSLPGQLGALTSQPLHRHGSDPGS
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Organism
Homo sapiens, Human
Protein Classification
Ion channel
>
Voltage-gated ion channel
>
Potassium channels
>
Voltage-gated potassium channel
Function
Pore-forming (alpha) subunit of voltage-gated inwardly rectifying potassium channel. Channel properties are modulated by cAMP and subunit assembly. Mediates the rapidly activating component of the delayed rectifying potassium current in heart (IKr) (PubMed:18559421, PubMed:26363003, PubMed:27916661).
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Uniprot ID
Primary ID:
Q12809

Secondarily ID:
A5H1P7
C4PFH9
D3DX04
O75418
O75680
Q708S9
Q9BT72
Q9BUT7
Q9H3P0
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HGNC ID
HGNC:6251
Subcellular Location
Cell membrane
Map of Molecular Bioactivity Related to the Protein
Map of Molecular Bioactivity Related to the Protein

Protein
Cell Line
Compound

Bioactivity Value:

<= 0.1 μM
> 0.1 μM and <= 10 μM
> 10 μM
Imprecise Activity
Table of Molecular Bioactivities Related to the Protein
Cell Line ID: CL000053 , COS-7
Compound ID Compound Name Compound Formula
CP0278751
BEPRIDIL HYDROCHLORIDE
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C24H34N2O
 1
1
IC50 = 550 nM
   TI
   LI
   LO
   TS
CP0013607
2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methyl-amino]ethyl]-6-fluoro-1-isopropyl-tetralin-2-yl] ester;hydrate;hydrochloride
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C29H38FN3O3
 1
1
IC50 = 1430 nM
   TI
   LI
   LO
   TS
Biochemical Assays
Compound ID Compound Name Compound Formula
CP0040184
1-[(4-fluorophenyl)methyl]-N-{1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl}-1H-1,3-benzodiazol-2-amine
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C28H31FN4O
 7
1 EC50 = 1.9 nM
2 IC50 = 0.9 nM
3 IC50 = 1.5 nM
4 IC50 = 3.31 nM
5 IC50 = 10 nM
6 IC50 = 11.48 nM
7 Ki = 20 nM
CP0218850
6-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-4H-1,4-benzoxazin-3-one
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C24H26N4O2
 2
1 EC50 = 7.943 nM
2 Ki = 63.1 nM
CP0052474
(4-{1-[2-(6-Methyl-pyridin-2-yl)-ethyl]-piperidine-4-carbonyl}-phenyl)-methanesulfonamide
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C21H27N3O3S
 8
1 EC50 = 25 nM
2 IC50 = 1.2 nM
3 IC50 = 7.82 nM
4 IC50 = 12.02 nM
5 IC50 = 19.95 nM
6 IC50 = 20 nM
7 IC50 = 21 nM
8 IC50 = 24.2 nM
CP0046703
1-(2-{4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
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C24H26ClFN4O
 4
1 IC50 = 3 nM
2 IC50 = 10 nM
3 IC50 = 14.7 nM
4 IC50 = 14.79 nM
CP0305866
1-(3-(4-(3-methylbenzo[b][1,4]oxathiin-2-yl)phenoxy)propyl)pyrrolidine
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C22H25NO2S
 1
1 IC50 = 4.4 nM
CP0253731
1-[3-[4-[(2R,3S)-3-methyl-2,3-dihydro-1,4-benzoxathiin-2-yl]phenoxy]propyl]pyrrolidine
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C22H27NO2S
 1
1 IC50 = 5 nM
CP0371449
1-(2-{4-[1-(4-Fluoro-phenyl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidine-2-thione
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C24H27FN4S
 1
1 IC50 = 6.166 nM
CP0030226
4-Amino-5-chloro-N-{1-[3-(4-fluoro-phenoxy)-propyl]-3-methoxy-piperidin-4-yl}-2-methoxy-benzamide
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C23H29ClFN3O4
 4
1 IC50 = 6.7 nM
2 IC50 = 6.761 nM
3 IC50 = 39.81 nM
4 IC50 = 47 nM
CP0171480
(Lu 23-086)1-(2-{4-[1-(4-Fluoro-phenyl)-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C24H27FN4O
 1
1 IC50 = 6.918 nM
CP0289652
7-fluoro-N-[1-[(3-fluoro-4-methoxyphenyl)methyl]piperidin-4-yl]-4-oxochromene-2-carboxamide
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C23H22F2N2O4
 1
1 IC50 = 8.5 nM
CP0356295
4-[2-[4-[2-(4-nitrophenyl)ethyl]piperazin-1-yl]ethyl]benzonitrile
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C21H24N4O2
 1
1 IC50 = 9 nM
CP0002229
(Dofetilide) N-[4-(2-{[2-(4-Methanesulfonylamino-phenyl)-ethyl]-methylamino}-ethoxy)-phenyl]-methanesulfonamide
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C19H27N3O5S2
 3
1 IC50 = 10 nM
2 IC50 = 30 nM
3 IC50 = 200 nM
CP0237326
N-[4-[4-[ethyl(heptyl)amino]-1-hydroxybutyl]phenyl]methanesulfonamide
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C20H36N2O3S
 3
1 IC50 = 10 nM
2 IC50 = 15.14 nM
3 IC50 = 20 nM
CP0198230
1-(2-{4-[5-Chloro-1-(4-fluoro-phenyl)-1H-indol-3-yl]-3,6-dihydro-2H-pyridin-1-yl}-ethyl)-imidazolidin-2-one
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C24H24ClFN4O
 1
1 IC50 = 10 nM
CP0008601
4-[4-(4-Chloro-phenyl)-4-hydroxy-piperidin-1-yl]-1-(4-fluoro-phenyl)-butan-1-one;propionate(HCl)
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C21H23ClFNO2
 5
1 IC50 = 10 nM
2 IC50 = 26.8 nM
3 IC50 = 26.92 nM
4 IC50 = 30.2 nM
5 IC50 = 1400 nM
CP0035258
N-methyl-3-phenyl-3-[4-(trifluoromethyl)phenoxy]propan-1-amine
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C17H18F3NO
 4
1 IC50 = 10 nM
2 IC50 = 457.09 nM
3 IC50 = 1513.56 nM
4 IC50 > 10000 nM
CP0036382
CAS_52-53-9
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C27H38N2O4
 4
1 IC50 = 10 nM
2 IC50 = 141.25 nM
3 IC50 = 400 nM
4 IC50 = 3100 nM
CP0041749
1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-2-benzofuran-5-carbonitrile
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C20H21FN2O
 2
1 IC50 = 10 nM
2 IC50 = 3981.07 nM
CP0292876
1-[5-chloro-1-(4-fluorophenyl)indol-3-yl]-N,N-dimethylmethanamine
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C17H16ClFN2
 1
1 IC50 = 10.96 nM
CP0253729
1-[3-[4-[(2R,3S)-3-ethyl-2,3-dihydro-1,4-benzoxathiin-2-yl]phenoxy]propyl]pyrrolidine
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C23H29NO2S
 1
1 IC50 = 11 nM
CP0648622
N-(4-(1-(2-(6-methylpyridin-2-yl)ethyl)piperidine-4-carbonyl)phenyl)methanesulfonamide dihydrochloride
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C21H29Cl2N3O3S
 2
1 IC50 = 11 nM
2 IC50 = 18.1 nM
CP0231382
1-[3-[4-[(2R,3S)-3-phenyl-2,3-dihydro-1,4-benzoxathiin-2-yl]phenoxy]propyl]pyrrolidine
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C27H29NO2S
 1
1 IC50 = 12 nM
CP0007317
(+)-(R)-2-(alpha-(2-(Diisopropylamino)ethyl)benzyl)-p-cresol
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C22H31NO
 1
1 IC50 = 16.98 nM
CP0027419
1-(1-(4,4-bis(4-fluorophenyl)butyl)piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
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C28H29F2N3O
 5
1 IC50 = 18 nM
2 IC50 = 50.12 nM
3 IC50 = 54.6 nM
4 IC50 = 54.95 nM
5 IC50 = 1700 nM
CP0311464
N-[1'-(6-cyano-1,2,3,4-tetrahydronaphthalen-2-yl)-4-hydroxyspiro[3,4-dihydrochromene-2,4'-piperidine]-6-yl]methanesulfonamide
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C25H29N3O4S
 1
1 IC50 = 20.89 nM
CP0278751
BEPRIDIL HYDROCHLORIDE
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C24H34N2O
 3
1 IC50 = 22.91 nM
2 IC50 = 430 nM
3 IC50 = 549.54 nM
CP0298427
1-(2-{4-[1-(4-Fluoro-phenyl)-2,3-dihydro-1H-indol-3-yl]-piperidin-1-yl}-ethyl)-imidazolidin-2-one
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C24H29FN4O
 1
1 IC50 = 23.44 nM
CP0282547
1-[3-[4-[(2R,3R)-3-methyl-2,3-dihydro-1,4-benzoxathiin-2-yl]phenoxy]propyl]pyrrolidine
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C22H27NO2S
 1
1 IC50 = 25 nM
CP0040487
1-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)-N-methyl-N-((tetrahydro-2H-pyran-4-yl)methyl)piperidin-4-amine
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C26H33FN4O
 1
1 IC50 = 29 nM
CP0264620
(S)-1-(2-(chroman-4-yl)ethyl)-4-(3,4-dimethoxyphenyl)piperidine
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C24H31NO3
 2
1 IC50 = 30 nM
2 IC50 = 251.19 nM
CP0163218
4-amino-5-chloro-N-[(3R,4S)-1-[3-(4-fluorophenoxy)propyl]-3-methoxypiperidin-4-yl]-2-methoxybenzamide
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C23H29ClFN3O4
 3
1 IC50 = 31.55 nM
2 IC50 = 270 nM
3 IC50 < 1000 nM
CP0040196
1-(1-(4-(4-fluorophenyl)-4-oxobutyl)-1,2,3,6-tetrahydropyridin-4-yl)-1H-benzo[d]imidazol-2(3H)-one
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C22H22FN3O2
 1
1 IC50 = 32.36 nM
CP0035893
(Thioridazine)10-[2-(1-Methyl-piperidin-2-yl)-ethyl]-2-methylsulfanyl-10H-phenothiazine
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C21H26N2S2
 4
1 IC50 = 33.2 nM
2 IC50 = 95.5 nM
3 IC50 = 190.55 nM
4 IC50 = 191 nM
CP0306020
4-(5-Chloro-3-{1-[2-(2-oxo-imidazolidin-1-yl)-ethyl]-piperidin-4-yl}-indol-1-yl)-benzoic acid methyl ester
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C26H29ClN4O3
 1
1 IC50 = 36.31 nM
CP0104272
1-[1,3-bis(chloranyl)-6-(trifluoromethyl)phenanthren-9-yl]-3-(dibutylamino)propan-1-ol;hydrochloride
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C26H30Cl2F3NO
 4
1 IC50 = 40 nM
2 IC50 = 156 nM
3 IC50 = 194.98 nM
4 IC50 = 199.53 nM
CP0033565
(+/-)1-(4-tert-butylphenyl)-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butan-1-ol
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C32H41NO2
 8
1 IC50 = 50 nM
2 IC50 = 56 nM
3 IC50 = 199.53 nM
4 IC50 = 213 nM
5 IC50 = 213.8 nM
6 Ki = 56 nM
7 Ki = 78 nM
8 Ki = 320 nM
CP0056747
4-[(4-Chlorophenyl)methyl]-2-({(2R)-1-[4-(4-{[3-(hexahydro-1H-azepin-1-yl)propyl]oxy}phenyl)butyl]-2-pyrrolidinyl}methyl)-1(2H)-phthalazinone
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C39H49ClN4O2
 1
1 IC50 = 50.12 nM
CP0237321
1-{2-[4-(5-Chloro-1-phenyl-1H-indol-3-yl)-piperidin-1-yl]-ethyl}-imidazolidin-2-one
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C24H27ClN4O
 1
1 IC50 = 87.1 nM
CP0294233
4-(4-Chloro-benzyl)-2-(1-methyl-azepan-4-yl)-2H-phthalazin-1-one
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C22H24ClN3O
 1
1 IC50 = 100 nM
CP0290006
(R)-2-(6-methyl-2-phenylpyrimidin-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C27H28N4
 1
1 IC50 = 120 nM
CP0056386
5-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)-6-chloroindolin-2-one
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C21H21ClN4OS
 4
1 IC50 = 120.23 nM
2 IC50 = 125 nM
3 IC50 = 125.89 nM
4 IC50 < 1000 nM
CP0530506
6-[[[1-[2-[6-methoxy-3-(trifluoromethyl)-1,5-naphthyridin-4-yl]ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H28F3N5O4
 1
1 IC50 = 130 nM
CP0029932
CHEMBL1614712
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C27H29N5O
 1
1 IC50 = 130 nM
CP0297101
methyl 2-[4-[5-chloro-3-[1-[2-(2-oxoimidazolidin-1-yl)ethyl]piperidin-4-yl]indol-1-yl]phenyl]acetate
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C27H31ClN4O3
 1
1 IC50 = 131.83 nM
CP0334084
1-{2-[4-(5-Chloro-1-cyclohexyl-1H-indol-3-yl)-piperidin-1-yl]-ethyl}-imidazolidin-2-one
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C24H33ClN4O
 1
1 IC50 = 138.04 nM
CP0039958
(risperidone)3-{2-[4-(6-Fluoro-benzo[d]isoxazol-3-yl)-piperidin-1-yl]-ethyl}-2-methyl-6,7,8,9-tetrahydro-pyrido[1,2-a]pyrimidin-4-one
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C23H27FN4O2
 7
1 IC50 = 147.91 nM
2 IC50 = 148 nM
3 IC50 = 167 nM
4 IC50 = 260 nM
5 IC50 = 778 nM
6 IC50 = 1070 nM
7 IC50 = 1330 nM
CP0077311
1-(3-(4-(5-chloro-2-oxo-2,3-dihydrobenzo[d]imidazol-1-yl)piperidin-1-yl)propyl)-1H-benzo[d]imidazol-2(3H)-one
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C22H24ClN5O2
 1
1 IC50 = 162.18 nM
CP0068895
ethyl 4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidine-1-carboxylate
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C22H23ClN2O2
 2
1 IC50 = 169.82 nM
2 IC50 = 173.78 nM
CP0232071
3-benzyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C29H31N3O2
 1
1 IC50 = 170 nM
CP0117618
2-fluoro-4-[2-[4-[2-(1-oxo-3H-2-benzofuran-5-yl)ethyl]piperazin-1-yl]ethyl]benzonitrile
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C23H24FN3O2
 1
1 IC50 = 170 nM
CP0045063
2-methyl-4-(4-methylpiperazin-1-yl)-10H-thieno[2,3-b][1,5]benzodiazepine
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C17H20N4S
 3
1 IC50 = 181 nM
2 IC50 = 181.97 nM
3 IC50 = 231.3 nM
CP0327634
1-(2-Chroman-4-yl-ethyl)-4-(3,4-dimethoxy-phenyl)-piperidine
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C24H31NO3
 1
1 IC50 = 199.53 nM
CP0110939
5-Chloro-1-(4-fluoro-phenyl)-3-piperidin-4-yl-1H-indole
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C19H18ClFN2
 1
1 IC50 = 204.17 nM
CP0347887
(5R)-31-oxo-20-oxa-2,6,11,13-tetraazahexacyclo[19.6.2.1^{2,5}.1^{15,19}.0^{9,13}.0^{24,28}]hentriaconta-1(27),9,11,15,17,19(30),21(29),22,24(28),25-decaene-18-carbonitrile
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C27H23N5O2
 1
1 IC50 = 210 nM
CP0356157
1-(4-chlorophenyl)-2-[3-(4-fluorophenoxy)propyl]guanidine
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C16H17ClFN3O
 1
1 IC50 = 216 nM
CP0040625
N-[3-[4-[4-[(4-methylphenyl)sulfonylamino]butyl]piperazin-1-yl]phenyl]acetamide
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C23H32N4O3S
 1
1 IC50 = 300 nM
CP0567161
6-[[[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-8-methyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H30FN5O4
 1
1 IC50 = 300 nM
CP0294516
10-(2-(1-methylpiperidin-2-yl)ethyl)-2-(methylsulfinyl)-10H-phenothiazine
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C21H26N2OS2
 3
1 IC50 = 316.23 nM
2 IC50 = 320 nM
3 IC50 = 549.54 nM
CP0025667
2-[4-(4-Methyl-benzyl)-piperazin-1-yl]-1-(2-methyl-2,3-dihydro-indol-1-yl)-ethanone
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C18H19ClN4
 5
1 IC50 = 320 nM
2 IC50 = 323.59 nM
3 IC50 = 901 nM
4 IC50 = 3200 nM
5 IC50 = 3981.07 nM
CP0003832
N'-hydroxy-N-phenyloctanediamide
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C14H20N2O3
 2
1 IC50 = 322 nM
2 IC50 > 30000 nM
CP0034615
(6-Methoxy-quinolin-4-yl)-(5-vinyl-1-aza-bicyclo[2.2.2]oct-2-yl)-methanol
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C20H24N2O2
 1
1 IC50 = 323.59 nM
CP0125124
1-Methyl-4-phenyl-piperidine-4-carboxylic acid ethyl ester
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C15H21NO2
 2
1 IC50 = 323.59 nM
2 IC50 = 74131.02 nM
CP0035515
(2R)-N-[6-(4-Chlorophenyl)-7-(2,4-dichlorophenyl)-2,2-dimethyl-3,4-dihydro-2H-pyrano[2,3-b]pyridine-4-yl]-2-hydroxypropanamide
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C25H23Cl3N2O3
 1
1 IC50 = 340 nM
CP0041757
1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol
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C24H26N2O4
 3
1 IC50 = 350 nM
2 IC50 = 10471.29 nM
3 IC50 = 12589.25 nM
CP0231514
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3-methyl-8-(trifluoromethyl)quinazolin-4(3H)-one
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C25H26F3N3O2
 1
1 IC50 = 350 nM
CP0313614
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-8-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 1
1 IC50 = 350 nM
CP0076698
(1R,3R)-1-(oxan-4-yl)-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
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C25H26N4O
 2
1 IC50 = 380 nM
2 Ki = 369 nM
CP0720695
Azimilide
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C23H28ClN5O3
 3
1 IC50 = 400 nM
2 IC50 = 562.34 nM
3 IC50 = 1412.54 nM
CP0046135
4-[2-[4-[2-(1-oxo-3H-2-benzofuran-5-yl)ethyl]piperazin-1-yl]ethyl]benzonitrile
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C23H25N3O2
 1
1 IC50 = 430 nM
CP0146498
2-((1-(1-(4-fluorobenzyl)-1H-benzo[d]imidazol-2-yl)piperidin-4-yl)(methyl)amino)pyrimidin-4(3H)-one
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C24H25FN6O
 1
1 IC50 = 436.52 nM
CP0002230
4-methyl-N-[3-(4-methyl-1H-imidazol-1-yl)-5-(trifluoromethyl)phenyl]-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino]benzamide
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C28H22F3N7O
 1
1 IC50 = 450 nM
CP0313890
4-[4-(Hydroxy-diphenyl-methyl)-piperidin-1-yl]-1-[4-(1-hydroxy-1-methyl-ethyl)-phenyl]-butan-1-ol
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C31H39NO3
 1
1 IC50 = 457.09 nM
CP0232074
3-phenyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C28H29N3O2
 1
1 IC50 = 460 nM
CP0042240
1-{3-[4-(3-Methyl-4,4-dioxo-4H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
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C22H25NO4S
 1
1 IC50 = 470 nM
CP0184098
2-(1-adamantyl)-1-(4-iodophenyl)guanidine
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C17H22IN3
 1
1 IC50 = 491.4 nM
CP0020486
6-methoxy-4-[2-[4-([1,3]oxathiolo[5,4-c]pyridin-6-ylmethylamino)piperidin-1-yl]ethyl]quinoline-3-carbonitrile
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C25H27N5O2S
 1
1 IC50 = 500 nM
CP0002211
N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-2-oxo-1H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
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C22H27FN4O2
 1
1 IC50 = 500 nM
CP0567047
6-[[[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-7,8-dimethyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C28H32FN5O4
 1
1 IC50 = 500 nM
CP0132905
Rilpivirine
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C22H18N6
 1
1 IC50 = 500 nM
CP0444610
CHEMBL4870418
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C24H23ClN4O
 1
1 IC50 = 500 nM
CP0070817
N-[(1-methylpiperidin-4-yl)methyl]-3-[3-(trifluoromethoxy)phenyl]imidazo[1,2-b]pyridazin-6-amine
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C20H22F3N5O
 3
1 IC50 = 511 nM
2 IC50 = 980 nM
3 IC50 = 1000 nM
CP0557813
CHEMBL4849414
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C22H20ClF2N3O
 1
1 IC50 = 520 nM
CP0177352
6-[[[1-[2-(6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C26H29N5O4
 1
1 IC50 = 560 nM
CP0170290
2-[4-[5-chloro-3-[1-[2-(2-oxoimidazolidin-1-yl)ethyl]piperidin-4-yl]indol-1-yl]phenyl]acetic acid
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C26H29ClN4O3
 1
1 IC50 = 575.44 nM
CP0013607
2-methoxyacetic acid [(1S,2S)-2-[2-[3-(1H-benzimidazol-2-yl)propyl-methyl-amino]ethyl]-6-fluoro-1-isopropyl-tetralin-2-yl] ester;hydrate;hydrochloride
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C29H38FN3O3
 4
1 IC50 = 580 nM
2 IC50 = 806 nM
3 IC50 = 1400 nM
4 IC50 = 1445.44 nM
CP0048052
4-(4-(2-(cyclopropylmethoxy)-5-(methylsulfonyl)benzoyl)piperazin-1-yl)-3-fluorobenzonitrile
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C23H24FN3O4S
 1
1 IC50 = 600 nM
CP0043996
(R)-2-(1-(3,4-dichlorophenyl)-5-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C26H26Cl2N4
 1
1 IC50 = 600 nM
CP0349959
1-cyclopropyl-3-[4-(1-phenylpyrrolo[2,3-c]pyridin-3-yl)pyridin-2-yl]urea
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C22H19N5O
 1
1 IC50 = 600 nM
CP0042927
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-3,4-dihydroquinolin-2(1H)-one
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C23H27Cl2N3O2
 5
1 IC50 = 630.96 nM
2 IC50 = 896.5 nM
3 IC50 = 3860 nM
4 IC50 < 1000 nM
5 Ki = 598 nM
CP0635260
eltrombopag
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C25H22N4O4
 1
1 IC50 = 690 nM
CP0231381
3-(4-{[3-(1-Pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C21H23N3O2
 1
1 IC50 = 710 nM
CP0240846
GS-333126
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C25H14F7N5
 1
1 IC50 = 794.33 nM
CP0011846
1-(2-(2-hydroxy-3-(propylamino)propoxy)phenyl)-3-phenylpropan-1-one
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C21H27NO3
 1
1 IC50 = 800 nM
CP0040489
1-(4-fluorobenzyl)-2-(4-(4-methyl-1H-pyrazol-1-yl)piperidin-1-yl)-1H-benzo[d]imidazole
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C23H24FN5
 1
1 IC50 = 809 nM
CP0000082
CAS_68647
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C18H19N3O
 1
1 IC50 = 812.83 nM
CP0165991
(R)-3-bromo-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)isoxazole
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C19H20BrN3O
 1
1 IC50 = 880 nM
CP0068493
(2-{4-[(2-butyl-1-benzofuran-3-yl)carbonyl]-2,6-diiodophenoxy}ethyl)diethylamine
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C25H29I2NO3
 2
1 IC50 = 1000 nM
2 IC50 = 10000 nM
CP0341378
(+/-)-1-{3-[4-(6-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
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C23H29NO5S
 1
1 IC50 = 1000 nM
CP0445227
6-[[[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-7-methyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H30FN5O4
 1
1 IC50 = 1000 nM
CP0087489
6-(4-(3,4-dimethoxybenzoyl)piperazin-1-yl)-3,4-dihydroquinolin-2(1H)-one
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C22H25N3O4
 2
1 IC50 = 1096.48 nM
2 IC50 = 18000 nM
CP0044035
1-(p-chlorophenyl)-1-(2-pyridyl)-3-N,N-dimethylpropylamine
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C16H19ClN2
 2
1 IC50 = 1100 nM
2 IC50 = 20892.96 nM
CP0232075
2-Phenyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C27H27N3O2
 1
1 IC50 = 1100 nM
CP0296278
8-chloro-2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3-methylquinazolin-4(3H)-one
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C24H26ClN3O2
 1
1 IC50 = 1100 nM
CP0007430
IBRUTINIB
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C25H24N6O2
 2
1 IC50 = 1100 nM
2 Ki = 1100 nM
CP0176864
CHEMBL4853672
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C24H22F2N4O
 1
1 IC50 = 1100 nM
CP0676878
6-((1-(2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)-2-oxoethyl)-2-oxabicyclo[2.2.2]octan-4-ylamino)methyl)-2H-pyrido[3,2-b][1,4]oxazin-3(4H)-one
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C26H26FN5O5
 1
1 IC50 = 1200 nM
CP0010656
3-(2-(4-(6-fluorobenzo[d]isoxazol-3-yl)piperidin-1-yl)ethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one
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C23H27FN4O3
 2
1 IC50 = 1288.25 nM
2 IC50 = 1300 nM
CP0343389
CHEMBL4846783
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C23H20F2N4O
 1
1 IC50 = 1300 nM
CP0093801
(R)-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-phenylthiazole
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C25H25N3S
 1
1 IC50 = 1360 nM
CP0055808
3-(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)-N-methylpropan-1-amine
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C18H22N2
 2
1 IC50 = 1380.38 nM
2 IC50 = 1390 nM
CP0074740
[(8R)-3-[2-(2,4-difluorophenyl)-1,3-thiazol-4-yl]-8-methyl-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone
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C26H19F2N5OS2
 1
1 IC50 = 1400 nM
CP0177354
6-[[[1-[2-[3-(hydroxymethyl)-6-methoxy-1,5-naphthyridin-4-yl]ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H31N5O5
 1
1 IC50 = 1440 nM
CP0033479
(chloropromazine) [3-(2-Chloro-phenothiazin-10-yl)-propyl]-dimethyl-amine
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C17H19ClN2S
 1
1 IC50 = 1479.11 nM
CP0151323
(R)-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(6-(2,2,2-trifluoroethoxy)pyridin-3-yl)thiazole
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C26H25F3N4OS
 1
1 IC50 = 1520 nM
CP0213280
6-[[[1-[2-(6-methoxy-3-methylsulfonyl-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H31N5O6S
 1
1 IC50 = 1550 nM
CP0142753
2,8-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 IC50 = 1600 nM
CP0164837
(R)-3-(4-chlorophenyl)-5-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)isoxazole
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C26H26ClN3O
 1
1 IC50 = 1600 nM
CP0194592
(R)-4-(2-(2-(2-methylpyrrolidin-1-yl)ethyl)benzofuran-5-yl)benzonitrile
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C22H22N2O
 1
1 IC50 = 1600 nM
CP0235590
(R)-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-phenylthiazole
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C25H25N3S
 1
1 IC50 = 1600 nM
CP0081096
2-methoxy-4-[2-[4-[2-(1-oxo-3H-2-benzofuran-5-yl)ethyl]piperazin-1-yl]ethyl]benzonitrile
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C24H27N3O3
 1
1 IC50 = 1600 nM
CP0479605
CHEMBL4845961
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C23H22ClF2N3O
 1
1 IC50 = 1600 nM
CP0194289
(S)-1-(6-((diethylamino)methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-(3-(trifluoromethyl)phenethyl)piperazin-2-one
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C28H36F3N3O
 1
1 IC50 = 1700 nM
CP0042239
(+/-)-1-{3-[4-(7-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
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C23H29NO5S
 1
1 IC50 = 1700 nM
CP0272546
3-ethyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C24H29N3O2
 1
1 IC50 = 1700 nM
CP0226201
(R)-3-methyl-2-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)benzo[d]thiazolo[3,2-a]imidazole
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C26H26N4S
 1
1 IC50 = 1720 nM
CP0296280
2-(4-(3-(piperidin-1-yl)propoxy)phenyl)-3-propylquinazolin-4(3H)-one
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C25H31N3O2
 1
1 IC50 = 1800 nM
CP0005212
US8987315, Ketoconazole
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C26H28Cl2N4O4
 2
1 IC50 = 1900 nM
2 IC50 = 1905.46 nM
CP0081972
(R)-N-(1-(3-(3,5-difluorophenyl)-3-(4-(methylsulfonyl)phenyl)propyl)piperidin-4-yl)-N-ethyl-2-(4-(methylsulfonyl)phenyl)acetamide
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C32H38F2N2O5S2
 2
1 IC50 = 1900 nM
2 IC50 = 7300 nM
CP0200768
CHEMBL85606
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C28H30N4O
 2
1 IC50 = 1995.26 nM
2 Ki = 630.96 nM
CP0043968
7-(2,5-dimethylpyrazol-3-yl)-3-[3-[[4-methyl-5-(2-methylquinolin-5-yl)-1,2,4-triazol-3-yl]sulfanyl]propyl]-1,2,4,5-tetrahydro-3-benzazepine
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C31H35N7S
 1
1 IC50 = 1995.26 nM
CP0013001
(+/-)-2-[(1-benzylpiperidin-4-yl)methyl]-5,6-dimethoxy-indan-1-one
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C24H29NO3
 1
1 IC50 = 1995.26 nM
CP0035188
(R)-2-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)benzo[d]thiazole
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C23H23N3S
 1
1 IC50 = 2000 nM
CP0142752
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3,8-dimethylquinazolin-4(3H)-one
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C25H29N3O2
 1
1 IC50 = 2000 nM
CP0191293
(R)-3-(4-chlorophenyl)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)isoxazole
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C26H26ClN3O
 1
1 IC50 = 2000 nM
CP0198938
(R)-2-(5'-methyl-2,2'-bithiophen-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H26N2S2
 1
1 IC50 = 2000 nM
CP0235588
(R)-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiophene-2-carbonitrile
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C21H21N3S
 1
1 IC50 = 2000 nM
CP0282425
1-[2-(3-chloro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-N-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)piperidin-4-amine
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C24H28ClN5O3
 1
1 IC50 = 2000 nM
CP0183196
6-[[[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C26H28FN5O4
 2
1 IC50 = 2000 nM
2 IC50 = 2100 nM
CP0420173
5-[2-[1-[2-[6-(tetrazol-1-yl)pyridin-3-yl]acetyl]piperidin-4-yl]ethyl]-3H-2-benzofuran-1-one
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C23H24N6O3
 1
1 IC50 = 2000 nM
CP0547955
CHEMBL4864639
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C24H25ClFN3O
 1
1 IC50 = 2050 nM
CP0069651
7-methoxy-N-(piperidin-4-ylmethyl)-3-[3-(trifluoromethoxy)phenyl]triazolo[4,5-b]pyridin-5-amine
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C19H21F3N6O2
 1
1 IC50 = 2100 nM
CP0547938
CHEMBL4863359
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C23H23Cl2N3O
 1
1 IC50 = 2300 nM
CP0534438
CHEMBL4861332
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C23H22ClF2N3O
 2
1 IC50 = 2400 nM
2 IC50 = 11000 nM
CP0029912
Aralen
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C18H26ClN3
 2
1 IC50 = 2500 nM
2 IC50 = 2511.89 nM
CP0218857
6-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 IC50 = 2500 nM
CP0232078
(+/-)-(S)-1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-3-methyl-piperidine
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C25H33NO5S
 1
1 IC50 = 2500 nM
CP0056899
(2-Benzhydryloxy-ethyl)-dimethyl-amine
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C17H21NO
 2
1 IC50 = 2570.4 nM
2 IC50 = 26915.35 nM
CP0064841
(2,8-Bis-trifluoromethyl-quinolin-4-yl)-(1-methyl-piperidin-2-yl)-methanol
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C17H16F6N2O
 3
1 IC50 = 2600 nM
2 IC50 = 5495.41 nM
3 IC50 = 5623.41 nM
CP0297753
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-7-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 1
1 IC50 = 2600 nM
CP0126643
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(4-(piperidin-1-yl)phenyl)quinoline
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C27H33N3
 1
1 IC50 = 2800 nM
CP0135721
2-(1-(2,4-difluorophenyl)-5-methyl-1H-1,2,3-triazol-4-yl)-6-(2-((R)-2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H25F2N5
 1
1 IC50 = 2800 nM
CP0202877
2-Propyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C24H29N3O2
 1
1 IC50 = 2800 nM
CP0219814
(R)-6-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazolo[3,2-b][1,2,4]triazole
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C21H23N5S
 1
1 IC50 = 2800 nM
CP0231379
3-methyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C23H27N3O2
 1
1 IC50 = 2800 nM
CP0072232
(R)-5-methyl-3-(4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazol-2-yl)isoxazole
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C23H24N4OS
 1
1 IC50 = 2840 nM
CP0102830
3-methyl-2-(4-(3-(pyrrolidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C22H25N3O2
 1
1 IC50 = 2900 nM
CP0253727
2-(4-(1-cyclopentylpiperidin-4-yloxy)phenyl)-3-methylquinazolin-4(3H)-one
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C25H29N3O2
 1
1 IC50 = 2900 nM
CP0282224
(+/-)-(R)-1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-2-methyl-pyrrolidine
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C24H31NO5S
 1
1 IC50 = 2900 nM
CP0305860
3-isopropyl-2-(4-(3-(piperidin-1-yl)propoxy)phenyl)quinazolin-4(3H)-one
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C25H31N3O2
 1
1 IC50 = 3000 nM
CP0048166
2-[[5-cyano-4-[2,4-dichloro-5-[2-(diethylamino)ethoxy]phenyl]-7H-pyrrolo[2,3-d]pyrimidin-2-yl]sulfanyl]-N-methylacetamide
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C22H24Cl2N6O2S
 1
1 IC50 = 3140 nM
CP0071568
5-methyl-2-[(5-methyl-1H-imidazol-4-yl)methyl]-3,4-dihydropyrid[4,3-b]indol-1-one;hydrochloride
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C17H18N4O
 2
1 IC50 = 3200 nM
2 IC50 = 3235.94 nM
CP0044008
(R)-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)benzonitrile
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C23H23N3
 1
1 IC50 = 3200 nM
CP0060491
10,11-dihydro-5-(gamma-dimethylaminopropylidene)-5H-dibenzo(a,d)cycloheptene
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C20H23N
 2
1 IC50 = 3290 nM
2 IC50 = 10000 nM
CP0045223
(S)-4-(4-chlorophenethyl)-1-(6-((diethylamino)-methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)piperazin-2-one
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C27H36ClN3O
 1
1 IC50 = 3300 nM
CP0010658
5-[2-ethoxy-5-(4-methyl-1-piperazinylsulfonyl)phenyl]-1-methyl-3-n-propyl-1,6-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one
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C22H30N6O4S
 2
1 IC50 = 3300 nM
2 IC50 = 3311.31 nM
CP0036757
3-(5,6-dihydrobenzo[b][1]benzazepin-11-yl)-N,N-dimethylpropan-1-amine
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C19H24N2
 1
1 IC50 = 3388.44 nM
CP0090824
(R)-2-(4H-benzo[d][1,3]dioxin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C24H26N2O2
 1
1 IC50 = 3600 nM
CP0282484
(R)-2-(6-chloropyridin-3-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H22ClN3
 1
1 IC50 = 3600 nM
CP0002793
(BRL 43694)1-Methyl-1H-indazole-3-carboxylic acid (9-methyl-9-aza-bicyclo[3.3.1]non-3-yl)-amide
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C18H24N4O
 2
1 IC50 = 3715.35 nM
2 IC50 = 3801.89 nM
CP0044093
(R)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(thiophen-2-yl)thiazole
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C24H25N3S2
 1
1 IC50 = 3720 nM
CP0039091
N-[3-[4-[4-(cyclohexylmethylsulfonylamino)butyl]piperazin-1-yl]phenyl]acetamide
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C23H38N4O3S
 2
1 IC50 = 3800 nM
2 Ki > 2000 nM
CP0042238
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-6-methoxy-3-methylquinazolin-4(3H)-one
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C25H29N3O3
 1
1 IC50 = 3800 nM
CP0231998
(+/-)-(S)-1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-2-methyl-pyrrolidine
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C24H31NO5S
 1
1 IC50 = 3800 nM
CP0179956
N-(piperidin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide
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C17H20F6N2O3
 1
1 IC50 = 3890.45 nM
CP0305864
2-Isopropyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C24H29N3O2
 1
1 IC50 = 3900 nM
CP0225649
2-amino-1-[3-(4-fluoroanilino)-2-(4-fluorophenyl)-6,8-dihydro-5H-imidazo[1,2-a]pyrazin-7-yl]-2-methylpropan-1-one
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C22H23F2N5O
 1
1 IC50 = 3950 nM
CP0062100
(-)-(R)-2-(1-(2-(2-(azetidin-1-yl)ethyl)benzo[b]thiophen-3-yl)ethyl)pyridine
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C20H22N2S
 1
1 IC50 = 4200 nM
CP0231378
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-7-methoxy-3-methylquinazolin-4(3H)-one
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C25H29N3O3
 1
1 IC50 = 4300 nM
CP0128076
8-Chloro-11-piperazin-1-yl-5H-dibenzo[b,e][1,4]diazepine
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C17H17ClN4
 2
1 IC50 = 4490 nM
2 IC50 = 31622.78 nM
CP0069452
5-[2-[4-[2-[4-(tetrazol-1-yl)phenyl]acetyl]piperazin-1-yl]ethyl]-3H-2-benzofuran-1-one
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C23H24N6O3
 2
1 IC50 = 4500 nM
2 IC50 = 14000 nM
CP0459494
5-[2-[4-[2-[6-(tetrazol-1-yl)pyridin-3-yl]acetyl]piperazin-1-yl]ethyl]-3H-2-benzofuran-1-one
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C22H23N7O3
 1
1 IC50 = 4500 nM
CP0027141
3-oxo-2-(2-pyridin-2-ylethyl)-N-[[4-(trifluoromethoxy)phenyl]methyl]-1H-isoindole-1-carboxamide
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C24H20F3N3O3
 1
1 IC50 = 4600 nM
CP0077040
4-Amino-5-chloro-2-ethoxy-N-[4-(4-fluoro-benzyl)-morpholin-2-ylmethyl]-benzamide; citrate(AS-4370)
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C21H25ClFN3O3
 1
1 IC50 = 4786.3 nM
CP0003146
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide
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C22H21Cl3N4O
 1
1 IC50 = 4800 nM
CP0073733
(+/-)-1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-piperidine
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C24H31NO5S
 1
1 IC50 = 4800 nM
CP0093794
(R)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(pyridin-4-yl)thiazole
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C25H26N4S
 1
1 IC50 = 4800 nM
CP0231698
(R)-ethyl 5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiophene-2-carbimidate
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C23H27N3OS
 1
1 IC50 = 4800 nM
CP0270573
2-Phenyl-3-piperidin-3-yl-1H-indole
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C19H20N2
 2
1 IC50 = 4897.79 nM
2 Ki = 4900 nM
CP0151774
1-{3-[4-((2S,3S)-8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
   Show/Hide
C23H29NO5S
 1
1 IC50 = 4900 nM
CP0170167
N-[4-[4-(2-methoxyphenyl)piperazin-1-yl]butyl]-4-methylbenzenesulfonamide
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C22H31N3O3S
 1
1 IC50 = 5000 nM
CP0291530
2-Ethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 IC50 = 5000 nM
CP0205340
N-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)-1-[2-(3-fluoro-6-methoxyquinolin-4-yl)ethyl]piperidin-4-amine
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C25H29FN4O3
 1
1 IC50 = 5000 nM
CP0658097
5-(1H-indol-7-ylamino)-3-((1R,2S)-2-aminocyclohexylamino)-1,2,4-triazine-6-carboxamide
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C18H22N8O
 1
1 IC50 = 5000 nM
CP0309072
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(1,2-thiazol-5-yl)-2,8-diazaspiro[4.5]decan-1-one
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C22H25N3O4S
 1
1 IC50 = 5000 nM
CP0367992
4-[3-[2-[[(4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-4-methyl-2-oxo-1,3-oxazolidin-3-yl]methyl]-4-(trifluoromethyl)phenyl]-4-chlorophenyl]-3-methylbenzoic acid
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C34H23ClF9NO4
 1
1 IC50 = 5000 nM
CP0126140
2-fluoro-N-[3-methoxy-4-[5-(3-piperidin-1-ylpropylamino)-1,3,4-oxadiazol-2-yl]phenyl]benzamide
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C24H28FN5O3
 2
1 IC50 = 5011.87 nM
2 IC50 = 16982.44 nM
CP0418474
CHEMBL4848514
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C24H23ClN4O
 1
1 IC50 = 5300 nM
CP0202876
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-3-methylquinazolin-4(3H)-one
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C24H27N3O2
 1
1 IC50 = 5600 nM
CP0177353
6-[[[1-[2-[3-(difluoromethyl)-6-methoxy-1,5-naphthyridin-4-yl]ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H29F2N5O4
 1
1 IC50 = 5850 nM
CP0073728
7-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 IC50 = 6000 nM
CP0238238
(R)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(pyridin-3-yl)thiazole
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C25H26N4S
 1
1 IC50 = 6000 nM
CP0271584
(R)-2-(5-chloro-1-methyl-3-phenyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C26H27ClN4
 1
1 IC50 = 6000 nM
CP0232076
1-{3-[4-((2R,3R)-8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
   Show/Hide
C23H29NO5S
 1
1 IC50 = 6200 nM
CP0253728
(+/-)-1-{3-[4-(5-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
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C23H29NO5S
 1
1 IC50 = 6300 nM
CP0185942
(R)-5-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-3-phenylisoxazole
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C26H27N3O
 1
1 IC50 = 6400 nM
CP0206060
2,5-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 IC50 = 6600 nM
CP0402857
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(3-methyl-1,2-thiazol-5-yl)-2,8-diazaspiro[4.5]decan-1-one
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C23H27N3O4S
 1
1 IC50 = 6600 nM
CP0074461
(2S,6R)-2,6-dimethyl-N-[4-[1-(oxan-4-yl)pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl]morpholine-4-carboxamide
   Show/Hide
C24H29N5O3
 1
1 IC50 = 6600 nM
CP0090649
2,7-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 IC50 = 6700 nM
CP0042236
(R)-2-tert-butyl-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C20H28N2
 1
1 IC50 = 6800 nM
CP0064169
5-hydroxy-2-(4-hydroxyphenyl)-N-methyl-4-(piperidin-1-ylmethyl)-1-benzofuran-3-carboxamide
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C22H24N2O4
 1
1 IC50 = 6900 nM
CP0780095
1-{3-[4-(8-Methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-propyl}-pyrrolidine
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C23H29NO5S
 1
1 IC50 = 7000 nM
CP0035807
Cocaine
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C17H21NO4
 1
1 IC50 = 7244.36 nM
CP0062495
(Z)-2-butenedioic acid;2-(2,2-dicyclohexylethyl)piperidine
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C19H35N
 1
1 IC50 = 7762.47 nM
CP0043999
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-8-fluoro-3-methylquinazolin-4(3H)-one
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C24H26FN3O2
 1
1 IC50 = 7900 nM
CP0350333
(3R,4S)-4-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethylamino)-1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]piperidin-3-ol
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C24H28FN5O4
 1
1 IC50 = 7900 nM
CP0191294
(R)-2-(2-methylimidazo[1,2-a]pyridin-3-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C24H26N4
 1
1 IC50 = 8000 nM
CP0114969
[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone
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C20H18N6OS2
 1
1 IC50 = 8000 nM
CP0062279
(S)-1-(6-((diethylamino)methyl)-1,2,3,4-tetrahydronaphthalen-2-yl)-4-(4-fluorophenethyl)piperazin-2-one
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C27H36FN3O
 1
1 IC50 = 8100 nM
CP0029449
(5S)-31-oxo-20-oxa-2,6,11,13-tetraazahexacyclo[19.6.2.1^{2,5}.1^{15,19}.0^{9,13}.0^{24,28}]hentriaconta-1(27),9,11,15,17,19(30),21(29),22,24(28),25-decaene-18-carbonitrile
   Show/Hide
C27H23N5O2
 1
1 IC50 = 8100 nM
CP0290003
5-Chloro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24ClN3O2
 1
1 IC50 = 8100 nM
CP0013593
1-(3-Hydroxy-propyl)-5-((R)-2-{2-[2-(2,2,2-trifluoro-ethoxy)-phenoxy]-ethylamino}-propyl)-2,3-dihydro-1H-indole-7-carboxylic acid amide
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C25H32F3N3O4
 1
1 IC50 = 8200 nM
CP0132553
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(2-methoxypyrimidin-4-yl)-2,8-diazaspiro[4.5]decan-1-one
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C24H28N4O5
 1
1 IC50 = 8200 nM
CP0219813
(R)-6-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)quinoxaline
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C24H24N4
 1
1 IC50 = 8400 nM
CP0004985
2-(4-fluorophenyl)-N-[6-methoxy-5-(4-methylimidazol-1-yl)pyridin-2-yl]-1-methylbenzimidazol-4-amine
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C24H21FN6O
 1
1 IC50 = 8500 nM
CP0093554
BIIB-057
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C19H23N9O
 2
1 IC50 = 8600 nM
2 IC50 = 9100 nM
CP0091000
(R)-2-(2,7-dimethylpyrazolo[1,5-a]pyrimidin-6-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C24H27N5
 1
1 IC50 = 8800 nM
CP0561521
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(3-methyl-1,2,4-thiadiazol-5-yl)-2,8-diazaspiro[4.5]decan-1-one
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C22H26N4O4S
 1
1 IC50 = 9000 nM
CP0016164
(3R,4R)-1-[3-(2,5-difluorophenyl)cyclobutyl]-4-[(3S)-3-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]piperidine-3-carboxylic acid
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C29H32F2N2O4
 1
1 IC50 = 9970 nM
CP0072374
BAY-E-5009
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C18H20N2O6
 1
1 IC50 = 10000 nM
CP0162544
5-tert-Butyl-1-(4-fluoro-phenyl)-1H-indole
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C18H18FN
 1
1 IC50 = 10000 nM
CP0224890
1-[5-Chloro-1-(4-fluoro-phenyl)-1H-indol-3-yl]-ethanone
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C16H11ClFNO
 1
1 IC50 = 10000 nM
CP0297102
5-Chloro-1-(4-fluoro-phenyl)-3-isopropyl-1H-indole
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C17H15ClFN
 1
1 IC50 = 10000 nM
CP0036394
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-8-methoxy-3-methylpyrido[3,4-d]pyrimidin-4(3H)-one
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C24H28N4O3
 1
1 IC50 = 10000 nM
CP0164197
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-5-(trifluoromethyl)-4(3H)-quinazolinone
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C23H24F3N3O2
 1
1 IC50 = 10000 nM
CP0206057
5-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 IC50 = 10000 nM
CP0206059
6-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O3
 1
1 IC50 = 10000 nM
CP0218851
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-8-methoxy-3-methylquinazolin-4(3H)-one
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C25H29N3O3
 1
1 IC50 = 10000 nM
CP0218853
2-(4-(1-cyclobutylpiperidin-4-yloxy)phenyl)-5-methoxy-3-methylquinazolin-4(3H)-one
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C25H29N3O3
 1
1 IC50 = 10000 nM
CP0231995
2,6-Dimethyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O2
 1
1 IC50 = 10000 nM
CP0296479
8-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone trifluoroacetate
   Show/Hide
C23H27N3O3
 1
1 IC50 = 10000 nM
CP0305862
8-Fluoro-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C22H24FN3O2
 1
1 IC50 = 10000 nM
CP0305863
5-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
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C23H27N3O3
 1
1 IC50 = 10000 nM
CP0305865
2-Methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
   Show/Hide
C22H25N3O2
 1
1 IC50 = 10000 nM
CP0310817
7-Methoxy-2-methyl-3-(4-{[3-(1-pyrrolidinyl)propyl]oxy}phenyl)-4(3H)-quinazolinone
   Show/Hide
C23H27N3O3
 1
1 IC50 = 10000 nM
CP0044706
(2E)-N-hydroxy-3-(4-{[(2-hydroxyethyl)[2-(1H-indol-3-yl)ethyl]amino]methyl}phenyl)prop-2-enamide
   Show/Hide
C22H25N3O3
 1
1 IC50 = 10300 nM
CP0455805
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(3-methoxy-1,2,4-thiadiazol-5-yl)-2,8-diazaspiro[4.5]decan-1-one
   Show/Hide
C22H26N4O5S
 1
1 IC50 = 10300 nM
CP0090976
(R)-2-(4-methyl-2-(pyrrolidin-1-yl)pyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
   Show/Hide
C25H31N5
 1
1 IC50 = 10400 nM
CP0198937
(R)-2-(1-(6-ethoxypyridazin-3-yl)-5-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
   Show/Hide
C26H30N6O
 1
1 IC50 = 10400 nM
CP0165503
2-amino-4-fluoro-5-(4-hydroxypiperidin-1-yl)sulfonyl-N-(3,4,5-trifluorophenyl)benzamide
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C18H17F4N3O4S
 1
1 IC50 = 10900 nM
CP0126599
N-[1-[(3R)-3-(3,5-difluorophenyl)-3-(1-methylsulfonylpiperidin-4-yl)propyl]piperidin-4-yl]-N-ethyl-2-(4-methylsulfonylphenyl)acetamide
   Show/Hide
C31H43F2N3O5S2
 1
1 IC50 = 11000 nM
CP0289830
(R)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(pyridin-2-yl)thiazole
   Show/Hide
C25H26N4S
 1
1 IC50 = 11200 nM
CP0165988
(R)-2-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazole
   Show/Hide
C19H21N3S
 1
1 IC50 = 11600 nM
CP0194663
7-[[[1-[[(3R)-5-fluoro-3-hydroxy-11-oxo-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-3-yl]methyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-1H-pyrido[3,4-b][1,4]oxazin-2-one
   Show/Hide
C26H26FN5O5
 1
1 IC50 = 11700 nM
CP0414064
5-[(1R)-1-hydroxy-2-[2-(5-methylsulfonylpyridin-2-yl)-2,8-diazaspiro[4.5]decan-8-yl]ethyl]-4-methyl-3H-2-benzofuran-1-one
   Show/Hide
C25H31N3O5S
 1
1 IC50 = 11700 nM
CP0049757
4-(diisopropylamino)-2-phenyl-2-pyridin-2-ylbutanamide
   Show/Hide
C21H29N3O
 2
1 IC50 = 12000 nM
2 IC50 = 91201.08 nM
CP0222016
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(pyridin-3-yl)quinoline
   Show/Hide
C21H23N3
 1
1 IC50 = 12000 nM
CP0264622
Anzemet Cinv
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C19H20N2O3
 1
1 IC50 = 12022.64 nM
CP0327633
MDL-74156
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C19H22N2O3
 1
1 IC50 = 12022.64 nM
CP0165987
(R)-2'-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2,4'-bithiazole
   Show/Hide
C23H24N4S2
 1
1 IC50 = 12400 nM
CP0100241
2-Methyl-10-piperazin-1-yl-4H-3-thia-4,9-diaza-benzo[f]azulene
   Show/Hide
C16H18N4S
 1
1 IC50 = 12589.25 nM
CP0209320
2-fluoro-N-[4-[5-(4-piperidin-1-ylbutylamino)-1,3,4-oxadiazol-2-yl]phenyl]benzamide
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C24H28FN5O2
 1
1 IC50 = 12589.25 nM
CP0095971
4-methyl-5-[2-[4-[2-[4-(tetrazol-1-yl)phenyl]acetyl]piperazin-1-yl]ethyl]-3H-2-benzofuran-1-one
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C24H26N6O3
 2
1 IC50 = 13000 nM
2 IC50 = 20000 nM
CP0088540
(+/-)-1-Cyclobutyl-4-[4-(8-methoxy-3-methyl-4,4-dioxo-3,4-dihydro-2H-4lambda*6*-benzo[1,4]oxathiin-2-yl)-phenoxy]-piperidine
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C25H31NO5S
 1
1 IC50 = 14000 nM
CP0145132
AZD7762
   Show/Hide
C17H19FN4O2S
 1
1 IC50 = 15000 nM
CP0312988
3-[5-Chloro-1-(4-fluoro-phenyl)-1H-indol-3-yl]-pentan-3-ol
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C19H19ClFNO
 1
1 IC50 = 15848.93 nM
CP0033646
AZD-9291
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C28H33N7O2
 1
1 IC50 = 16200 nM
CP0091072
(R)-2-(5-methyl-1-(6-methyl-4-(trifluoromethyl)pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C27H28F3N5
 1
1 IC50 = 16800 nM
CP0046632
US9056859, 72
   Show/Hide
C23H25N7O3
 1
1 IC50 = 17000 nM
CP0077731
(+)-cis-Diltiazem
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C22H26N2O4S
 1
1 IC50 = 17378.01 nM
CP0567159
6-[[[1-[2-[6-(2-aminoethoxy)-3-fluoro-1,5-naphthyridin-4-yl]ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H31FN6O4
 1
1 IC50 = 17500 nM
CP0090975
(R)-2-(3-methyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C20H24N4
 1
1 IC50 = 17600 nM
CP0218860
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(pyridin-2-yl)quinoline
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C21H23N3
 1
1 IC50 = 18000 nM
CP0232572
(R)-N,N-dimethyl-6-(5-methyl-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1H-pyrazol-1-yl)pyridazin-3-amine
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C26H31N7
 1
1 IC50 = 18000 nM
CP0082827
AT-4140
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C19H22F2N4O3
 1
1 IC50 = 18197.01 nM
CP0146499
2-fluoro-N-[3-fluoro-4-[5-(4-morpholin-4-ylbutylamino)-1,3,4-oxadiazol-2-yl]phenyl]benzamide
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C23H25F2N5O3
 1
1 IC50 = 18620.87 nM
CP0361823
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-pyridin-4-yl-2,8-diazaspiro[4.5]decan-1-one
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C24H27N3O4
 1
1 IC50 = 19500 nM
CP0181333
US9206199, 22
   Show/Hide
C24H25N7O4
 1
1 IC50 = 19700 nM
CP0024122
(3R,4R)-4-[(3S)-3-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-(2-thiophen-2-ylsulfanylethyl)piperidine-3-carboxylic acid
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C25H30N2O4S2
 2
1 IC50 = 19700 nM
2 IC50 = 21000 nM
CP0044007
(R)-1-(4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)phenyl)pyridin-4(1H)-one
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C27H27N3O
 1
1 IC50 = 20000 nM
CP0044094
(R)-2-(5-methyl-1-(pyridin-2-yl)-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C25H27N5
 1
1 IC50 = 20000 nM
CP0126641
(R)-2-(2,6-dimethylpyridin-3-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C23H27N3
 1
1 IC50 = 20000 nM
CP0309069
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(1-methyl-6-oxopyridazin-3-yl)-2,8-diazaspiro[4.5]decan-1-one
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C24H28N4O5
 2
1 IC50 = 20000 nM
2 IC50 > 90000 nM
CP0073725
(R)-2,4-dimethyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazole
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C21H25N3S
 1
1 IC50 = 20400 nM
CP0091071
(R)-2-(2,6-dichloropyridin-4-yl)-4-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazole
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C24H22Cl2N4S
 1
1 IC50 = 20400 nM
CP0242688
(R)-4-(4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)thiazol-2-yl)morpholine
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C24H30N4OS
 1
1 IC50 = 20400 nM
CP0160930
PILSICAINIDE
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C17H24N2O
 1
1 IC50 = 20417.38 nM
CP0090825
(R)-2-([1,2,4]triazolo[1,5-a]pyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H22N6
 1
1 IC50 = 20800 nM
CP0376890
5-[1-fluoro-2-[4-[2-[6-(tetrazol-1-yl)pyridin-3-yl]acetyl]piperazin-1-yl]ethyl]-4-methyl-3H-2-benzofuran-1-one
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C23H24FN7O3
 1
1 IC50 = 22000 nM
CP0689663
5-(((3R,4R)-3-aminotetrahydro-2H-pyran-4-yl)amino)-3-(4-methoxy-1H-indol-2-yl)pyrazine-2-carboxamide
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C19H22N6O3
 1
1 IC50 = 22000 nM
CP0189728
US9018211, 2A
   Show/Hide
C26H30N2O6
 2
1 IC50 = 22000 nM
2 IC50 = 23000 nM
CP0686385
(S)-3-(4-(3-(4-chlorobenzyl)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)piperidin-1-yl)-1H-1,2,4-triazol-5-amine
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C23H27ClN6O
 1
1 IC50 = 22000 nM
CP0165984
(R)-2-(4-methylpiperidin-1-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C22H31N3
 1
1 IC50 = 22400 nM
CP0216065
(R)-2-(2-methoxypyrimidin-5-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H24N4O
 1
1 IC50 = 22400 nM
CP0441184
5-[(1R)-1-hydroxy-2-[2-(5-methylsulfonylpyrazin-2-yl)-2,8-diazaspiro[4.5]decan-8-yl]ethyl]-4-methyl-3H-2-benzofuran-1-one
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C24H30N4O5S
 1
1 IC50 = 22700 nM
CP0025032
2-(4-{1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidin-1-yl]butyl}phenyl)-2-methylpropanoic acid
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C32H39NO4
 2
1 IC50 = 22908.68 nM
2 Ki = 23000 nM
CP0011242
(3R,4R)-4-[(3S)-3-(3-fluoro-6-methoxyquinolin-4-yl)-3-hydroxypropyl]-1-(2-thiophen-2-ylsulfanylethyl)piperidine-3-carboxylic acid
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C25H29FN2O4S2
 1
1 IC50 = 23600 nM
CP0088854
[(8R)-8-methyl-3-(2-methyl-1,3-thiazol-4-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-(4-thiophen-2-ylphenyl)methanone
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C21H19N5OS2
 1
1 IC50 = 24000 nM
CP0051541
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(5-methylsulfonylpyridin-2-yl)-2,8-diazaspiro[4.5]decan-3-one
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C25H29N3O6S
 1
1 IC50 = 24000 nM
CP0349958
N-[4-[1-(oxan-4-yl)pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl]morpholine-4-carboxamide
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C22H25N5O3
 1
1 IC50 = 24100 nM
CP0126642
(R)-2-(1,3-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H26N4
 1
1 IC50 = 24800 nM
CP0126699
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(pyrazin-2-yl)quinoline
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C20H22N4
 1
1 IC50 = 24800 nM
CP0183353
6-[[(3R,4R)-3-aminooxan-4-yl]amino]-8-(1H-indol-7-ylamino)-2H-2,7-naphthyridin-1-one
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C21H22N6O2
 1
1 IC50 = 24900 nM
CP0017287
(3R,4R)-4-[(3S)-3-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]-1-(3-phenylcyclobutyl)piperidine-3-carboxylic acid
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C29H34N2O4
 1
1 IC50 = 24900 nM
CP0184986
6-[[[1-[2-[3-fluoro-6-(2-hydroxyethoxy)-1,5-naphthyridin-4-yl]ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H30FN5O5
 1
1 IC50 = 25000 nM
CP0337894
(1R)-2-[4-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethylamino)piperidin-1-yl]-1-(6-methoxy-1,5-naphthyridin-4-yl)ethanol
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C24H29N5O4
 1
1 IC50 = 25100 nM
CP0091001
(R)-2-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-4,5-dihydrothiazole
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C19H23N3S
 1
1 IC50 = 25200 nM
CP0058434
6-[[[1-[(1S)-2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)-1-hydroxyethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C26H28FN5O5
 1
1 IC50 = 26000 nM
CP0232570
(R)-2-(6-methylpyridin-3-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C22H25N3
 1
1 IC50 = 26400 nM
CP0366397
6-[[[1-[2-(6-methoxy-3-methyl-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H31N5O4
 1
1 IC50 = 27430 nM
CP0051539
8-[(2R)-2-hydroxy-2-(4-methyl-1-oxo-3H-2-benzofuran-5-yl)ethyl]-2-(5-methylsulfonylpyrazin-2-yl)-2,8-diazaspiro[4.5]decan-3-one
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C24H28N4O6S
 1
1 IC50 = 27800 nM
CP0135717
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(pyridin-4-yl)quinoline
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C21H23N3
 1
1 IC50 = 28000 nM
CP0124168
2-fluoro-N-[4-[5-(4-morpholin-4-ylbutylamino)-1,3,4-oxadiazol-2-yl]phenyl]benzamide
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C23H26FN5O3
 1
1 IC50 = 29512.09 nM
CP0389764
5-[(1R)-1-hydroxy-2-[2-(6-methylsulfonylpyridin-3-yl)-2,8-diazaspiro[4.5]decan-8-yl]ethyl]-4-methyl-3H-2-benzofuran-1-one
   Show/Hide
C25H31N3O5S
 1
1 IC50 = 29600 nM
CP0366449
6-[[[1-[(1S)-2-[3-fluoro-6-(2-hydroxyethoxy)-1,5-naphthyridin-4-yl]-1-hydroxyethyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
   Show/Hide
C27H30FN5O6
 1
1 IC50 = 29700 nM
CP0358870
4-methyl-5-[1-[4-[2-[6-(tetrazol-1-yl)pyridin-3-yl]acetyl]piperazin-1-yl]propan-2-yl]-3H-2-benzofuran-1-one
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C24H27N7O3
 1
1 IC50 = 30000 nM
CP0150720
2-(2-{4-[(4-chlorophenyl)(phenyl)methyl]piperazin-1-yl}ethoxy)acetic acid
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C21H25ClN2O3
 2
1 IC50 = 30199.52 nM
2 IC50 = 31622.78 nM
CP0242687
(R)-4-methyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(pyrazin-2-yl)thiazole
   Show/Hide
C24H25N5S
 1
1 IC50 = 32000 nM
CP0055087
(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione
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C37H67NO13
 1
1 IC50 = 39000 nM
CP0230989
3-[4-[(3S)-3-[(4-chlorophenyl)methyl]morpholin-4-yl]piperidin-1-yl]-1H-1,2,4-triazol-5-amine
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C18H25ClN6O
 1
1 IC50 = 39000 nM
CP0044006
(R)-2-methyl-3-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-1,8-naphthyridine
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C25H26N4
 1
1 IC50 = 40000 nM
CP0090662
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
   Show/Hide
C16H20N2
 1
1 IC50 = 40000 nM
CP0090980
(R)-2-(3,5-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
   Show/Hide
C21H26N4
 1
1 IC50 = 40000 nM
CP0091002
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(1H-pyrazol-5-yl)quinoline
   Show/Hide
C19H22N4
 1
1 IC50 = 40000 nM
CP0206064
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(pyrimidin-5-yl)quinoline
   Show/Hide
C20H22N4
 1
1 IC50 = 40000 nM
CP0218968
(R)-2-(1,5-dimethyl-1H-pyrazol-4-yl)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C21H26N4
 1
1 IC50 = 40000 nM
CP0232571
(R)-3-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2-(trifluoromethyl)pyridin-4-ol
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C22H22F3N3O
 1
1 IC50 = 40000 nM
CP0232574
(R)-6-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-2,3-dihydroimidazo[2,1-b]thiazole
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C21H24N4S
 1
1 IC50 = 40000 nM
CP0232575
(R)-6-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)-[1,3]dioxolo[4,5-b]pyridine
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C22H23N3O2
 1
1 IC50 = 40000 nM
CP0232579
(R)-6-(2-(2-methylpyrrolidin-1-yl)ethyl)-2-(1H-pyrazol-4-yl)quinoline
   Show/Hide
C19H22N4
 1
1 IC50 = 40000 nM
CP0253726
(R)-2,4-dimethyl-5-(6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinolin-2-yl)oxazole
   Show/Hide
C21H25N3O
 1
1 IC50 = 40000 nM
CP0567336
(1S,2S)-2-[[7-fluoro-8-[2-[4-[(3-oxo-4H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]ethyl]-1,5-naphthyridin-2-yl]oxymethyl]cyclopropane-1-carboxylic acid
   Show/Hide
C30H32FN5O6
 1
1 IC50 = 43400 nM
CP0222014
(R)-2-cyclopropyl-6-(2-(2-methylpyrrolidin-1-yl)ethyl)quinoline
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C19H24N2
 1
1 IC50 = 44000 nM
CP0181203
1-[2-[4-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethylamino)piperidin-1-yl]ethyl]-2-oxoquinoline-7-carbonitrile
   Show/Hide
C25H27N5O3
 1
1 IC50 = 44000 nM
CP0133264
A-56268
   Show/Hide
C38H69NO13
 2
1 IC50 = 46000 nM
2 IC50 = 58884.37 nM
CP0027239
(3R,4R)-1-[3-(2,6-difluorophenyl)cyclobutyl]-4-[(3S)-3-hydroxy-3-(6-methoxyquinolin-4-yl)propyl]piperidine-3-carboxylic acid
   Show/Hide
C29H32F2N2O4
 1
1 IC50 = 47600 nM
CP0052206
1-Cyclopropyl-6-fluoro-5-methyl-7-(3-methyl-piperazin-1-yl)-4-oxo-1,4,4a,8a-tetrahydro-quinoline-3-carboxylic acid (Grepafloxacin)
   Show/Hide
C19H22FN3O3
 2
1 IC50 = 50000 nM
2 IC50 = 50118.72 nM
CP0126108
(4-fluorophenyl)-[(8R)-8-(2-hydroxyethyl)-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
   Show/Hide
C17H17FN6O2S
 1
1 IC50 = 50000 nM
CP0147959
[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-phenylmethanone
   Show/Hide
C16H16N6OS
 1
1 IC50 = 50000 nM
CP0046619
Adalat
   Show/Hide
C17H18N2O6
 1
1 IC50 = 50118.72 nM
CP0108552
4-methyl-5-[2-[4-[2-[3-methyl-5-(tetrazol-1-yl)pyridin-2-yl]acetyl]piperazin-1-yl]ethyl]-3H-2-benzofuran-1-one
   Show/Hide
C24H27N7O3
 1
1 IC50 = 52000 nM
CP0237307
US9206199, 21
   Show/Hide
C24H25N7O4
 1
1 IC50 = 56500 nM
CP0212153
(4-chlorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
   Show/Hide
C16H15ClN6OS
 1
1 IC50 = 66000 nM
CP0002800
1-((p-(2-(5-chloro-o-anisamido)ethyl)phenyl)sulfonyl)-3-cyclohexylurea
   Show/Hide
C23H28ClN3O5S
 2
1 IC50 = 74000 nM
2 IC50 = 74131.02 nM
CP0322115
4-(5-Chloro-3-{1-[2-(2-oxo-imidazolidin-1-yl)-ethyl]-piperidin-4-yl}-indol-1-yl)-benzoic acid
   Show/Hide
C25H27ClN4O3
 1
1 IC50 = 74131.02 nM
CP0333449
US9206199, 23
   Show/Hide
C24H25N7O4
 1
1 IC50 = 74900 nM
CP0205342
(1R)-2-[4-(2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-ylmethylamino)piperidin-1-yl]-1-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethanol
   Show/Hide
C24H28FN5O4
 1
1 IC50 = 79400 nM
CP0308131
9,13b-dihydro-1H-dibenzo[c,f]imidazo[1,5-a]azepin-3-amine
   Show/Hide
C16H15N3
 1
1 IC50 = 91201.08 nM
CP0039577
9-phenyl-8-(4-((4-(5-(pyridin-2-yl)-1H-1,2,4-triazol-3-yl)piperidin-1-yl)methyl)phenyl)-[1,2,4]triazolo[3,4-f][1,6]naphthyridine
   Show/Hide
C34H29N9
 1
1 IC50 > 10000 nM
CP0049926
(R)-2-(4-cyclopropylphenyl)-N-(1-(5-(2,2,2-trifluoroethoxy)pyridin-2-yl)ethyl)acetamide
   Show/Hide
C20H21F3N2O2
 1
1 IC50 > 10000 nM
CP0134600
5-(4-methylsulfonylphenyl)-3-[6-(trifluoromethyl)pyridin-3-yl]pyridin-2-amine
   Show/Hide
C18H14F3N3O2S
 1
1 IC50 > 10000 nM
CP0262055
N-[3-[(2S,5R)-6-amino-5-ethylsulfonyl-2-(fluoromethyl)-5-methyl-3,4-dihydropyridin-2-yl]-4-fluorophenyl]-2,2-difluoro-[1,3]dioxolo[4,5-c]pyridine-6-carboxamide
   Show/Hide
C22H22F4N4O5S
 1
1 IC50 > 10000 nM
CP0057972
2-[[4-(2-chloro-4,5-dimethoxyphenyl)-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-2-yl]sulfanyl]-N,N-dimethylacetamide
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C19H18ClN5O3S
 1
1 IC50 > 30000 nM
CP0086081
2-[[4-(2-chloro-5-hydroxy-4-methoxyphenyl)-5-cyano-7H-pyrrolo[2,3-d]pyrimidin-2-yl]sulfanyl]-N,N-dimethylacetamide
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C18H16ClN5O3S
 1
1 IC50 > 30000 nM
CP0118574
7-[[(1R,2S)-2-aminocyclohexyl]amino]-5-(1H-indol-7-ylamino)-3H-pyrido[4,3-d]pyrimidin-4-one
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C21H23N7O
 1
1 IC50 > 30000 nM
CP0068661
CHEMBL3355987
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C21H25ClN4O
 1
1 IC50 > 30000 nM
CP0114551
CHEMBL3355552
   Show/Hide
C22H25F3N4O
 1
1 IC50 > 30000 nM
CP0114708
CHEMBL3355544
   Show/Hide
C19H19F3N4O2
 1
1 IC50 > 30000 nM
CP0177776
CHEMBL3355550
   Show/Hide
C19H19F3N4O
 1
1 IC50 > 30000 nM
CP0074483
4-ethyl-N-[4-[1-(oxan-4-yl)pyrrolo[2,3-c]pyridin-3-yl]pyridin-2-yl]piperazine-1-carboxamide
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C24H30N6O2
 1
1 IC50 > 30000 nM
CP0270792
CHEMBL4640031
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C26H33N5O3
 1
1 IC50 > 30000 nM
CP0390388
1-(oxan-4-yl)-3-pyridin-4-ylpyrrolo[2,3-c]pyridine
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C17H17N3O
 1
1 IC50 > 30000 nM
CP0042443
(S)-1-(5-phenyl-3-(piperidin-3-ylcarbamoyl)thiophen-2-yl)urea
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C17H20N4O2S
 1
1 IC50 > 31600 nM
CP0098301
1-[(1R,2R)-1,2-diphenyl-2-piperidin-1-ylethyl]piperidine
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C24H32N2
 1
1 IC50 > 33000 nM
CP0123212
(3R)-3-[[4-[(5-chloro-2,3-dihydro-1,4-benzodioxin-6-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H27ClFN3O5
 1
1 IC50 > 60000 nM
CP0194662
6-[[[1-[[(3R)-5-fluoro-3-hydroxy-11-oxo-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-3-yl]methyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-7-methyl-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C27H28FN5O5
 1
1 IC50 > 60000 nM
CP0194683
(3R)-3-[[4-[(8-chloro-2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H26ClFN4O5
 1
1 IC50 > 60000 nM
CP0194684
(3R)-5-fluoro-3-hydroxy-3-[[4-(1,2,3,4-tetrahydropyrido[2,3-b]pyrazin-6-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H29FN6O3
 1
1 IC50 > 60000 nM
CP0257060
(3R)-5-fluoro-3-hydroxy-3-[[4-[(3-methyl-2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H29FN4O5
 1
1 IC50 > 60000 nM
CP0257224
(3R)-3-[[4-(1,3-benzodioxol-5-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H26FN3O5
 1
1 IC50 > 60000 nM
CP0257248
(3R)-5-fluoro-3-[[4-[(6-fluoro-2,3-dihydro-1,4-benzodioxin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H27F2N3O5
 1
1 IC50 > 60000 nM
CP0286018
(3R)-5-fluoro-3-hydroxy-3-[[4-[(2-methyl-2,3-dihydro-[1,4]dioxino[2,3-c]pyridin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H29FN4O5
 1
1 IC50 > 60000 nM
CP0286019
(3R)-3-[[4-[(1,1-dioxo-2,3-dihydro-[1,4]oxathiino[2,3-c]pyridin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H27FN4O6S
 1
1 IC50 > 60000 nM
CP0286020
(3R)-5-fluoro-3-hydroxy-3-[[4-[(4-methyl-2,3-dihydropyrido[3,2-b][1,4]oxazin-6-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H30FN5O4
 1
1 IC50 > 60000 nM
CP0347527
(3R)-3-[[4-(6,7-dihydro-[1,4]dioxino[2,3-c]pyridazin-3-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C25H26FN5O5
 1
1 IC50 > 60000 nM
CP0362596
7-[[[1-[[(3R)-5-fluoro-3-hydroxy-11-oxo-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-3-yl]methyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-2,3-dihydro-[1,4]dioxino[2,3-c]pyridine-8-carbonitrile
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C27H26FN5O5
 1
1 IC50 > 60000 nM
CP0367924
(3R)-3-[[4-[(5,8-dichloro-2,3-dihydro-1,4-benzodioxin-6-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H26Cl2FN3O5
 1
1 IC50 > 60000 nM
CP0463213
(3R)-3-[[4-[(6-chloro-2,3-dihydro-1,4-benzodioxin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H27ClFN3O5
 1
1 IC50 > 60000 nM
CP0511464
(3R)-3-[[4-(2,3-dihydro-[1,4]dioxino[2,3-b]pyridin-6-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H27FN4O5
 1
1 IC50 > 60000 nM
CP0511465
(3R)-3-[[4-(3,4-dihydro-2H-pyrido[3,2-b][1,4]oxazin-6-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H28FN5O4
 1
1 IC50 > 60000 nM
CP0557192
(3R)-3-[[4-(2,3-dihydro-1,4-benzodioxin-6-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C27H28FN3O5
 1
1 IC50 > 60000 nM
CP0560825
7-ethyl-6-[[[1-[[(3R)-5-fluoro-3-hydroxy-11-oxo-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-3-yl]methyl]-2-oxabicyclo[2.2.2]octan-4-yl]amino]methyl]-4H-pyrido[3,2-b][1,4]oxazin-3-one
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C28H30FN5O5
 1
1 IC50 > 60000 nM
CP0560826
(3R)-3-[[4-(2,3-dihydro-[1,4]oxathiino[3,2-c]pyridin-7-ylmethylamino)-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H27FN4O4S
 1
1 IC50 > 60000 nM
CP0566821
(3R)-3-[[4-[(4,4-dioxo-2,3-dihydro-[1,4]oxathiino[3,2-c]pyridin-7-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]methyl]-5-fluoro-3-hydroxy-1,7-diazatricyclo[6.3.1.04,12]dodeca-4(12),5,7,9-tetraen-11-one
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C26H27FN4O6S
 1
1 IC50 > 60000 nM
CP0272596
N-[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]-N-methyl-3-oxo-4H-pyrido[3,2-b][1,4]oxazine-6-carboxamide
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C27H28FN5O5
 1
1 IC50 > 60000 nM
CP0453242
N-[1-[2-(3-fluoro-6-methoxy-1,5-naphthyridin-4-yl)ethyl]-2-oxabicyclo[2.2.2]octan-4-yl]-3-oxo-4H-pyrido[3,2-b][1,4]oxazine-6-carboxamide
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C26H26FN5O5
 1
1 IC50 > 60000 nM
CP0528791
(1R,2S)-2-[[7-fluoro-8-[2-[4-[(3-oxo-4H-pyrido[3,2-b][1,4]oxazin-6-yl)methylamino]-2-oxabicyclo[2.2.2]octan-1-yl]ethyl]-1,5-naphthyridin-2-yl]oxymethyl]cyclopropane-1-carboxylic acid
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C30H32FN5O6
 1
1 IC50 > 60000 nM
CP0066063
N-[2-[[(1S,2R,4R)-2-(benzenesulfonylmethyl)-4-[methyl(propan-2-yl)amino]cyclohexyl]amino]-2-oxoethyl]-3-(trifluoromethyl)benzamide
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C27H34F3N3O4S
 1
1 IC50 > 80000 nM
CP0188530
6-(4-chlorophenyl)-3-[6-(4-hydroxypiperidin-1-yl)pyridin-3-yl]pyrrolo[2,1-f][1,2,4]triazin-4-one
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C22H20ClN5O2
 1
1 IC50 > 80000 nM
CP0112422
(4-fluorophenyl)-[(8R)-8-methyl-3-(3-methyl-1,2,4-thiadiazol-5-yl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]methanone
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C16H15FN6OS
 1
1 IC50 > 100000 nM
CP0002598
US9493448, 122
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C20H21ClFN5O3S
 1
1 IC50 > 100000 nM
CP0538171
1-({4-[4-chloro-2-(5-chloro-pyridin-2-ylcarbamoyl)-phenylcarbamoyl]-phenyl}-imino-methyl)-piperidine-3-carboxylic acid ethyl ester
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C28H27Cl2N5O4
 1
1 Ki = 16 nM
CP0371094
1'-(2,4-difluorophenethyl)-6-methoxyspiro[3,4-dihydro-2H-chromene-2,4'-(hexahydropyridine)]
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C22H25F2NO2
 1
1 Ki = 20 nM
CP0447444
1'-(2,4-difluorophenethyl)spiro[1,2,3,4-tetrahydronaphthalene-2,4'-(hexahydropyridine)]
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C22H25F2N
 1
1 Ki = 69 nM
CP0345223
3-(1-Phenethyl-piperidin-4-yl)-2-phenyl-1H-indole
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C27H28N2
 1
1 Ki = 80 nM
CP0045013
(3R)-1-cyclohexyl-3-(5-phenyl-1H-imidazol-2-yl)-2,3,4,9-tetrahydro-1H-pyrido[3,4-b]indole
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C26H28N4
 1
1 Ki = 80 nM
CP0039097
1'-(2,4-difluorophenethyl)spiro[3,4-dihydro-2H-chromene-2,4'-(hexahydropyridine)]
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C21H23F2NO
 1
1 Ki = 110 nM
CP0891260
(3R,4R)-6-Fluoro-3-(4-fluoropiperidin-3-yl)-2-naphthalen-2-yl-1H-indole
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C23H20F2N2
 1
1 Ki = 110 nM
CP0091025
5-chloro-N-(5-chloro-pyridin-2-yl)-2-[4-(N,N-dimethyl-carbamimidoyl)-benzoylamino]-benzamide
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C22H19Cl2N5O2
 1
1 Ki = 110 nM
CP0511470
4-(4-Chloro-benzenesulfonyl)-1-[2-(2,4-difluoro-phenyl)-ethyl]-piperidine
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C19H20ClF2NO2S
 1
1 Ki = 150 nM
CP0094782
2-{3-[4-(4-Fluoro-phenyl)-piperazin-1-yl]-propyl}-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide
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C23H24FN3O2S
 1
1 Ki = 200 nM
CP0304607
N-[2-[(5-chloropyridin-2-yl)carbamoyl]-4-methoxyphenyl]-4-(N,N-dimethylcarbamimidoyl)-2-piperidin-1-ylbenzamide
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C28H31ClN6O3
 1
1 Ki = 200 nM
CP0262775
3-(1-Benzyl-piperidin-3-yl)-2-phenyl-1H-indole
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C26H26N2
 1
1 Ki = 290 nM
CP0829637
(3R,4R)-6-Fluoro-3-(4-fluoropiperidin-3-yl)-2-naphthalen-1-yl-1H-indole
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C23H20F2N2
 1
1 Ki = 500 nM
CP0347876
3-(1-(2-Phenylethyl)piperidin-3-yl)-2-phenyl-1H-indole
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C27H28N2
 1
1 Ki = 530 nM
CP0347888
4-[[1-(2-(2,4-Difluorophenyl)ethyl)-4-piperidinyl]sulfonyl]benzonitrile
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C20H20F2N2O2S
 1
1 Ki = 560 nM
CP0345192
1'-[2-(2,4-Difluorophenyl)ethyl]-3,4-dihydrospiro[2H-1-benzothiopyran-2,4'-piperidine]-1,1-dioxide
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C21H23F2NO2S
 1
1 Ki = 570 nM
CP0044329
1-(2,4-difluorophenethyl)-4-(4-fluorophenylsulfonyl)piperidine
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C19H20F3NO2S
 1
1 Ki = 710 nM
CP0126585
4-methyl-6-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-1,4-benzoxazin-3-one
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C25H28N4O2
 1
1 Ki = 794.33 nM
CP0701507
(3R,4R)-6-Fluoro-3-(4-fluoropiperidin-3-yl)-1H-indole-2-carboxylic acid phenylamide
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C20H19F2N3O
 1
1 Ki = 930 nM
CP0040626
1-(2,4-difluorophenethyl)-4-(phenylsulfonyl)piperidine
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C19H21F2NO2S
 1
1 Ki = 1000 nM
CP0075436
(2,3-Dimethoxy-phenyl)-{1-[2-(4-fluoro-phenyl)-ethyl]-piperidin-4-yl}-methanol
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C22H28FNO3
 1
1 Ki = 1100 nM
CP0746305
3-((3R,4R)-4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
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C19H19FN2
 1
1 Ki = 1100 nM
CP0371095
1'-phenethylspiro[1,2,3,4-tetrahydronaphthalene-2,4'-(hexahydropyridine)]-1-ol; hydrochloride
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C22H27NO
 1
1 Ki = 1200 nM
CP0311380
6-Fluoro-2-(4-fluoro-phenyl)-3-piperidin-3-yl-1H-indole
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C19H18F2N2
 1
1 Ki = 1300 nM
CP0371096
4-[[1-(2-(2,4-Difluorophenyl)ethyl)-4-piperidinyl]sulfonyl]benzamide
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C20H22F2N2O3S
 1
1 Ki = 1300 nM
CP0647510
(3R,4R)-6-Chloro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
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C19H18ClFN2
 1
1 Ki = 1400 nM
CP0829638
(3R,4R)-6-Fluoro-3-(4-fluoropiperidin-3-yl)-2-thiophen-3-yl-1H-indole
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C17H16F2N2S
 1
1 Ki = 1500 nM
CP0844291
(3R,4R)-6-Fluoro-2-(4-fluorophenyl)-3-(4-fluoropiperidin-3-yl)-1H-indole
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C19H17F3N2
 1
1 Ki = 1600 nM
CP0039099
1-(2-Phenylethyl)-4-(phenylsulfonyl)piperidine
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C19H23NO2S
 1
1 Ki = 1800 nM
CP0037570
BEVYXXA
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C23H22ClN5O3
 1
1 Ki = 1800 nM
CP0430154
3-[[1-(2-(2,4-Difluorophenyl)ethyl)-4-piperidinyl]sulfonyl]benzonitrile
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C20H20F2N2O2S
 1
1 Ki = 1900 nM
CP0826952
(3R,4R)-7-Chloro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
   Show/Hide
C19H18ClFN2
 1
1 Ki = 2100 nM
CP0042313
N-[2-[(5-chloropyridin-2-yl)carbamoyl]-4-methoxyphenyl]-4-(N,N-dimethylcarbamimidoyl)-2-fluorobenzamide
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C23H21ClFN5O3
 1
1 Ki = 2100 nM
CP0289001
1-(3-Phenylpropyl)-4-(phenylsulfonyl)piperidine
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C20H25NO2S
 1
1 Ki = 2500 nM
CP0916293
(3R,4R)-6-Fluoro-3-(4-fluoro-piperidin-3-yl)-2-pyridin-3-yl-1H-indole
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C18H17F2N3
 1
1 Ki = 2500 nM
CP0275239
(-)-(R)-2-(3-(1-(5-fluoropyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C19H21FN2S
 1
1 Ki = 2500 nM
CP0283739
8-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-4H-1,4-benzoxazin-3-one
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C24H26N4O2
 1
1 Ki = 2511.89 nM
CP0907832
(3R,4R)-7-Fluoro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
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C19H18F2N2
 1
1 Ki = 3000 nM
CP0040490
(R)-1-(4-fluorobenzyl)-2-(1-methylpiperidin-3-yl)-1H-benzo[d]imidazole
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C20H22FN3
 1
1 Ki = 3900 nM
CP0270386
4-methyl-8-[2-[4-(2-methylquinolin-5-yl)piperazin-1-yl]ethyl]-1,4-benzoxazin-3-one
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C25H28N4O2
 1
1 Ki = 3981.07 nM
CP0039100
2-[[1-(2-(2,4-Difluorophenyl)ethyl)-4-piperidinyl]sulfonyl]benzonitrile
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C20H20F2N2O2S
 1
1 Ki = 4000 nM
CP0802170
6-Fluoro-3-(4-fluoro-piperidin-3-yl)-2-phenyl-1H-indole
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C19H18F2N2
 1
1 Ki = 4000 nM
CP0647511
2-Cyclohexyl-3-(4-fluoro-piperidin-3-yl)-1H-indole
   Show/Hide
C19H24F2N2
 1
1 Ki = 5400 nM
CP0152373
1-(2,4-difluorophenethyl)-4-fluoro-4-(4-fluorophenylsulfonyl)piperidine
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C19H19F4NO2S
 1
1 Ki = 5561 nM
CP0245025
2-Phenyl-3-piperidin-4-yl-1H-indole
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C19H20N2
 1
1 Ki = 5700 nM
CP0039034
2-(1-methylpiperidin-3-yl)-1-(2-phenoxyethyl)-1H-benzo[d]imidazole
   Show/Hide
C21H25N3O
 1
1 Ki = 5900 nM
CP0245024
1-(4-Fluorophenyl)-2-[4-(phenylsulfonyl)-1-piperidinyl]-ethanone
   Show/Hide
C19H20FNO3S
 1
1 Ki = 6800 nM
CP0311378
3-(1-Methyl-piperidin-2-yl)-2-phenyl-1H-indole
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C20H22N2
 1
1 Ki = 7000 nM
CP0816404
(3R,4R)-5-Fluoro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
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C19H18F2N2
 1
1 Ki = 7000 nM
CP0816405
(3R,4R)-5-Chloro-3-(4-fluoropiperidin-3-yl)-2-phenyl-1H-indole
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C19H18ClFN2
 1
1 Ki = 7000 nM
CP0345222
3-[[1-(2-(2,4-Difluorophenyl)ethyl)-4-piperidinyl]sulfonyl]benzamide
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C20H22F2N2O3S
 1
1 Ki = 7143.01 nM
CP0844290
(3R,4R)-6-Fluoro-3-(4-fluoropiperidin-3-yl)-1H-indole-2-carboxylic Acid Methyl Ester
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C15H16F2N2O2
 1
1 Ki = 8200 nM
CP0371098
3-(1-Methyl-piperidin-3-yl)-2-phenyl-1H-indole
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C20H22N2
 1
1 Ki = 9599.99 nM
CP0036238
(-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)ethanamine
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C19H22N2S
 1
1 Ki > 5 nM
CP0056536
N,N-dimethyl-2-[3-(pyrazin-2-ylmethyl)-1H-inden-2-yl]ethanamine
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C18H21N3
 1
1 Ki > 3000 nM
CP0101717
(-)-Dimethyl-{2-[3-((R)-1-pyrazin-2-yl-ethyl)-1H-inden-2-yl]-ethyl}-amine
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C19H23N3
 1
1 Ki > 3000 nM
CP0092749
(-)-(R)-N,N-dimethyl-2-(3-(1-(pyridin-3-yl)ethyl)benzo[b]thiophen-2-yl)ethanamine
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C19H22N2S
 1
1 Ki > 5000 nM
CP0147331
(-)-(R)-N-methyl-2-(3-(1-(pyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)ethanamine
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C18H20N2S
 1
1 Ki > 5000 nM
CP0147381
(-)-(R)-N,N-dimethyl-2-(3-(1-(3-methylpyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)ethanamine
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C20H24N2S
 1
1 Ki > 5000 nM
CP0156538
(-)-(R)-2-(3-(1-(2-fluoropyridin-3-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C19H21FN2S
 1
1 Ki > 5000 nM
CP0156608
(-)-(S)-2-(3-(1-(2-chloropyridin-3-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C19H21ClN2S
 1
1 Ki > 5000 nM
CP0204086
(-)-(R)-2-(3-(1-(1H-pyrazol-1-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C17H21N3S
 1
1 Ki > 5000 nM
CP0214258
(-)-(R)-2-(3-(1-(3-fluoropyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C19H21FN2S
 1
1 Ki > 5000 nM
CP0214261
(+)-(R)-2-(3-(1-(3-methoxypyridin-2-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C20H24N2OS
 1
1 Ki > 5000 nM
CP0244950
(-)-(R)-2-(3-(1-(2-methoxypyridin-3-yl)ethyl)benzo[b]thiophen-2-yl)-N,N-dimethylethanamine
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C20H24N2OS
 1
1 Ki > 5000 nM
CP0275228
(-)-(R)-N,N-dimethyl-2-(3-(1-(thiazol-4-yl)ethyl)benzo[b]thiophen-2-yl)ethanamine
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C17H20N2S2
 1
1 Ki > 5000 nM
CP0099167
(4-(2,4-difluorophenethyl)piperidin-1-yl)(2-fluorophenyl)methanone
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C20H20F3NO
 1
1 Ki > 9000 nM
CP0042315
1-(2-(2-(5-chloropyridin-2-ylcarbamoyl)-4-methoxyphenylcarbamoyl)-5-(N,N-dimethylcarbamimidoyl)phenyl)piperidine-4-carboxylic acid
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C29H31ClN6O5
 1
1 Ki > 10000 nM
CP0163484
2-(3-(5-chloropyridin-2-ylcarbamoyl)-4-(4-(N,N-dimethylcarbamimidoyl)benzamido)phenoxy)acetic acid
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C24H22ClN5O5
 1
1 Ki > 10000 nM
CP0065988
1-(4-fluorobenzyl)-2-(1-methylpiperidin-3-yl)-1H-benzo[d]imidazole
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C20H22FN3
 1
1 Ki > 10000 nM
CP0134298
1-({4-[4-chloro-2-(5-chloro-pyridin-2-ylcarbamoyl)-phenylcarbamoyl]-phenyl}-imino-methyl)-piperidine-3-carboxylic acid
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C26H23Cl2N5O4
 1
1 Ki > 10000 nM
CP0208472
N-(2-amino-5-thiophen-2-ylphenyl)-6-(2-oxo-1-oxa-3,8-diazaspiro[4.5]decan-8-yl)pyridine-3-carboxamide
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C23H23N5O3S
 1
1 Ki > 30000 nM
Clinical Information about the Protein
Target 1 ( Voltage-gated potassium channel Kv11.1 (KCNH2) )
Target Type Successful Target
Disease 6 Target-related Diseases  6
1 Cardiac failure [ICD-11: BD10-BD13]
2 Sleep-wake disorder [ICD-11: 7A00-7B2Z]
3 Pain [ICD-11: MG30-MG3Z]
4 Malaria [ICD-11: 1F40-1F45]
5 Cardiac arrhythmias [ICD-11: BC9Z]
6 Ovarian cancer [ICD-11: 2C73]
Approved Drug(s) 1 Approved Drug  1
1 VESNARINONE Approved
Cardiac failure
Clinical Trial Drug(s) 4 Clinical Trial Drugs  4
1 M100907 Phase 3
Sleep-wake disorder
2 ABT-229 Phase 2
Pain
3 NITD609 Phase 2
Malaria
4 ISOQUINE Phase 1
Malaria
Discontinued Drug(s) 1 Discontinued Drug  1
1 MK-499 Discontinued in Phase 2
Cardiac arrhythmias
Investigative Drug(s) 1 Investigative Drug  1
1 6-(4-CHLOROPHENYL)-7-(2,4-DICHLOROPHENYL)-N-(HYDROXYMETHYL)-1,2,2-TRIMETHYL-1,2,3,4-TETRAHYDRO-1,8-NAPHTHYRIDINE-4-CARBOXAMIDE (ENANTIOMERIC MIX) Investigative
Ovarian cancer
Similar Protein(s) and Bioactivity Statistics
50% Identity
Protein ID Protein Name Protein Organism
PT06976 Potassium voltage-gated channel subfamily H member 2 Canis lupus familiaris, Dog, Canis familiaris